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Active ingredients
Enalapril
Release form
Pills
Composition
enalapril maleate 2.5 mg; Excipients: maleic acid, anhydrous lactose, zinc stearate.
Pharmacological effect
Antihypertensive drug, ACE inhibitor. The mechanism of action is associated with inhibition of ACE activity, which leads to a decrease in the formation of angiotensin II. Enalapril belongs to prodrugs: after its hydrolysis, enalaprilat is formed in the body, which inhibits this enzyme. Enalapril also has some diuretic effect .; Along with a decrease in blood pressure, the drug reduces the pre- and afterload on the myocardium for heart failure, improves blood circulation in the small circle and respiratory function, reduces resistance in the kidney vessels, which helps normalize blood circulation in them .; Duration of action is 12-24 h.
Pharmacokinetics
Absorption; After taking the drug inside enalapril is rapidly and fairly fully absorbed from the gastrointestinal tract. Cmax in plasma is reached after 3-4 hours. Bioavailability of the drug is 53-74% .; Distribution; Plasma protein binding - 50% .; Metabolism; Enalapril is metabolized in the liver, a part is hydrolyzed to enalaprilat, therefore, in patients with impaired liver function, the time of maximum action may be increased .; Excretion; excreted by the kidneys. T1 / 2 is about 11 hours.
Indications
- arterial hypertension (including renovascular hypertension) .; - chronic heart failure (as part of combination therapy).
Contraindications
- an indication of a history of angioedema associated with treatment with ACE inhibitors; - aortic stenosis; - mitral stenosis; - pregnancy; - lactation period; - childhood; - Hypersensitivity to enalapril and other ACE inhibitors.
Use during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation.
Dosage and administration
Enam is prescribed for oral administration regardless of the meal time .; For patients not receiving diuretics, an initial dose of 5 mg / day is recommended. Further, the dose is selected individually .; A dose of 10–40 mg / day in 1 or 2 doses is usually required .; For patients receiving diuretics in order to prevent arterial hypotension, the diuretic should be canceled 1-2 days before the appointment of therapy.If diuretic cannot be discontinued, an initial dose of Enama 2.5 mg is recommended. In chronic heart failure, it is preferable to start treatment with a dose of 2.5 mg 1 time per day. Requires constant monitoring of blood pressure. Then it is recommended to take 25 mg 2 times / day for 3-4 days .; Starting from the second week, the dose, if necessary, increase to 10 mg 1 time / day. At 3-4 weeks, the dose is increased to 20 mg in 1 or 2 doses, if the systolic pressure is not lower than 100 mm Hg. v .; Selection of the dose and further treatment can be carried out on an outpatient basis, it is necessary to evaluate the patient's condition at least 1 time per month (only when selecting the dose, examination and monitoring of the doctor is required every 10 days), to monitor the content of creatinine and electrolytes in the blood. The presence of arterial hypotension to 80/60 mm Hg. st. against the background of maintenance therapy in the absence of complaints in a patient is not a reason for discontinuation of the drug. With care to apply along with diuretics (especially "loopback" and potassium-sparing), as well as with potassium preparations. With the development of arterial hypotension, the patient should be transferred to bed rest for several days, if this does not help, then the patient should be poured into / in 400-800 ml of physiological saline .; In hypertension caused by nephropathy in patients with diabetes mellitus, the dose of the drug depends on whether or not diabetic nephropathy is accompanied by arterial hypertension. If diabetic nephropathy occurs on the background of normal blood pressure, Enam is prescribed in small doses - 2.5 or 5 mg / day. If nephropathy is accompanied by arterial hypertension, the doses are selected in the same way as in arterial hypertension (up to a maximum of 40 mg / day) .; In case of renal insufficiency with a CC of more than 30 ml / min (the content of serum creatinine is not more than 3 mg / dL), it is recommended to prescribe the drug in the usual dose. When CC is less than 30 ml / min, the initial dose is not more than 2.5 mg / day. Further, the dose is selected individually under the control of the level of creatinine and blood electrolytes. For patients on hemodialysis, the initial dose and the dose on dialysis days should not exceed 2.5 mg / day.
Side effects
From the side of the central nervous system: 2-3% - headache, dizziness, fatigue; very rarely when used in high doses - insomnia, increased nervous irritability,depression, imbalance, paresthesia, tinnitus .; On the part of the respiratory system: 2-3% - dry cough, shortness of breath .; On the part of the digestive system: less than 2% - nausea, diarrhea; rarely - pancreatitis, liver failure, dyspeptic symptoms, dry mouth, abdominal pain .; Since the cardiovascular system: arterial hypotension, syncope; very rarely - cardiac arrhythmia, angina pectoris .; Changes in laboratory parameters: proteinuria, hyperkalemia, increased activity of hepatic transaminases, increased concentration of bilirubin in the blood, neutropenia, decreased hemoglobin, hematocrit and / or leukocytes .; Allergic reactions: skin rash; in some cases - angioedema of the face, larynx .; Other: very rarely when used in high doses - hair loss, hot flashes, glossitis, impotence; in patients with autoimmune diseases - agranulocytosis .; Enam is generally well tolerated and in most cases does not cause adverse reactions requiring discontinuation of the drug.
Overdose
Symptoms: arterial hypotension .; Treatment: should put the patient, lift the legs. In mild cases of overdose, the patient is prescribed a saline solution. In more serious cases, in the conditions of a hospital, measures are taken to stabilize blood pressure, saline or plasma substitutes are injected. Perhaps the use of hemodialysis.
Interaction with other drugs
With the simultaneous appointment of Enam with NSAIDs, the hypotensive effect of enalapril may be reduced; with potassium-sparing diuretics (spironolactone, triamterene, amiloride) - hyperkalemia may develop; with lithium salts - slowing down the elimination of lithium (shown to control the concentration of lithium in the blood plasma) .; Ethanol enhances the hypotensive effect of the drug .; With simultaneous use with antipyretic and analgesic drugs may reduce the effectiveness of Enam .; Enalapril weakens the effect of drugs containing theophylline .; Cimetidine lengthens the action of enalapril .; Simultaneous use with diuretics, beta-blockers, methyldopa, nitrates, calcium channel blockers, hydralazine, prazosin enhances the hypotensive effect of enalapril .; The use of Ename with anesthetics with antihypertensive effects can cause arterial hypotension
special instructions
After the appointment of Enam, it is possible to increase the level of urea nitrogen and serum creatinine due to the development of arterial hypotension and secondary renal hypoperfusion .; In appointing Enam, the previous therapy with diuretics and potassium preparations should be revised. 2 weeks after the appointment of Enam, it is necessary to monitor the laboratory parameters: urea nitrogen, creatinine and plasma electrolytes, as well as urinalysis; With extreme caution and under the supervision of a physician, the drug should be used with a combination of chronic heart failure or arterial hypertension with bilateral renal artery stenosis or arterial stenosis of a single kidney .; The development of arterial hypotension is not a reason to discontinue the drug, but it requires compliance with preventive measures (control of blood electrolytes, control of blood pressure, dose adjustment of the drug) .; Enam prevents potassium loss, so when it is prescribed it is not necessary to use potassium-saving diuretics and potassium preparations. Otherwise, hyperkalemia may develop, especially in patients with renal insufficiency and diabetes mellitus .; Before examining the function of the parathyroid glands, Enam should be canceled .; During the period of treatment is prohibited to drink alcohol.